scholarly journals UPLC-ESI-MS/MS Profile and Antioxidant, Cytotoxic, Antidiabetic, and Antiobesity Activities of the Aqueous Extracts of Three Different Hibiscus Species

2020 ◽  
Vol 2020 ◽  
pp. 1-17
Author(s):  
Hanan M. Al-Yousef ◽  
Wafaa H. B. Hassan ◽  
Sahar Abdelaziz ◽  
Musarat Amina ◽  
Rasha Adel ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Aqueous Extract ◽  
Biological Activities ◽  
Biological Effects ◽  
Aqueous Extracts ◽  
Potent Effect ◽  
Esi Ms ◽  
Biological Studies ◽  
Hct 116

The aqueous extracts of Hibiscus calyphyllus (HcA), Hibiscus micranthus (HmA), and Hibiscus deflersii (HdA) growing in Saudi Arabia did not receive enough attention in phytochemical and biological studies. This inspired the authors to investigate the phytochemicals of these extracts for the first time using UPLC-ESI-MS/MS in negative and positive ionization modes. The analysis afforded the tentative identification of 103 compounds including phenolic compounds, flavonoids, and anthocyanins. Moreover, in vitro evaluations of their cytotoxic, antioxidant, antidiabetic, and antiobesity activities were carried out. The results showed that aqueous extract of Hibiscus calyphyllus had the highest activity as an antioxidant agent (SC50 = 111 ± 1.5 μg/mL) compared with ascorbic acid (SC50 = 14.2 ± 0.5 μg/mL). MTT assay was used to evaluate cytotoxic activity compared to cisplatin. Hibiscus deflersii showed the most potent cytotoxic effect against A-549 (human lung carcinoma) with IC50 = 50 ± 5.1 μg/mL, and Hibiscus micranthus showed a close effect with IC50 = 60.4 ± 1.7 μg/mL. Hibiscus micranthus showed the most potent effect on HCT-116 (human colon carcinoma) with IC50 = 56 ± 1.9 μg/mL compared with cisplatin (IC50 = 7.53 ± 3.8 μg/mL). HcA and HdA extracts showed weak cytotoxic activity against A-549 and HCT-116 cell lines compared to the other extracts. Eventually, Hibiscus deflersii showed astonishing antidiabetic (IC50 = 56 ± 1.9 μg/mL) and antiobesity (IC50 = 95.45 ± 1.9 μg/mL) activities using in vitro α-amylase inhibitory assay (compared with acarbose (IC50 = 34.71 ± 0.7 μg/mL)) and pancreatic lipase inhibitory assay (compared with orlistat (IC50 = 23.8 ± 0.7 μg/mL)), respectively. In conclusion, these findings are regarded as the first vision of the phytochemical constituents and biological activities of different Hibiscus aqueous extracts. Hibiscus deflersii aqueous extract might be a hopeful origin of functional constituents with anticancer (on A-549 cell line), antidiabetic, and antiobesity activities. It might be a natural alternative remedy and nutritional policy for diabetes and obesity treatment without negative side effects. Isolation of the bioactive phytochemicals from the aqueous extracts of aerial parts of Hibiscus calyphyllus, Hibiscus micranthus, and Hibiscus deflersii and estimation of their biological effects are recommended in further studies.

Synthesis of New Cyanopyridine Scaffolds and their Biological Activities

2020 ◽  
Vol 17 (7) ◽  
pp. 567-575
Author(s):  
Nabil A. Alhakamy ◽  
Ahmad O. Noor ◽  
Khaled M. Hosny ◽  
Jenny Jeehan Nasr ◽  
Moustafa M.G. Fouda ◽  
...  
Keyword(s):  
Vitamin C ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Biological Effects ◽  
Tuberculosis H37rv ◽  
Cytotoxic Agents ◽  
H37rv Strain ◽  
Dpph Method

Background: 3-Cyanopyridine analogues are significant moieties with a variety of biological effects such as antioxidant, antimicrobial, anti-inflammatory and cytotoxic agents. In addition, they could be applied in the treatment of several diseases. Objective: The study conducted cyclo-addition of 3a-e derivatives with malononitrile to yield the corresponding 6-(4-((3-cyano-pyridinyl) amino) phenyl)-4-phenylnicotinonitriles 4a-e. Materials and Methods: Physical and spectral analyses were performed to demonstrate the proper structures of all incorporated analogues. The in vitro antimicrobial activity of the preps derivatives was investigated by testing them with a panel of pathogenic strains of bacteria and fungi. The anti-tuberculosis activity was observed against the Mycobacterium tuberculosis H37Rv strain. When examining cytotoxic agents for four different cell lines, researchers found that their activity was persuasive compared with that of standard antibiotics. In addition, the antioxidant activity of the synthesized analogues was evaluated using the DPPH method. Results and Discussions: The synthesized analogues were examined to determine their activity against the M. tuberculosis H37Rv strain. Derivatives 2c, 2e, 3d and 3e had good inhibition. Further screening was done for the highest potency against M. tuberculosis to determine the MICs. The antioxidant efficacy was evaluated via the DPPH technique matched with vitamin C as a positive control. The prospective results showed that the derivatives did not display scavenging efficacies in comparison with the standard. Conclusion: Some synthesized derivatives displayed good potency against bacterial activity and M. Tuberculosis. However, the antioxidant performance of these derivatives did not display scavenging efficacies compared to vitamin C. The cytotoxic activity of the synthesized derivatives was examined against various cell lines to display good cytotoxic activity in the order 4a-e > 2a-e > 3a-b.

Evaluation of Pyrano[3,2 C] Quinoline Analogues as Anticancer Agents

2019 ◽  
Vol 19 (10) ◽  
pp. 1285-1292 ◽  
Author(s):  
Kuldip D. Upadhyay ◽  
Anamik K. Shah
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Tumor Growth Inhibition ◽  
Mice Model ◽  
One Pot ◽  
Aryl Ring ◽  
Hct 116

Background: Quinoline analogues exhibited diversified biological activities depending on the structure type. A number of natural products with pyrano[3,2-c]quinolone structural motifs and patented chromenes were reported as promising cytotoxic agents. Objective: The present study is aimed to evaluate a new series of pyrano[3,2-c]quinoline scaffolds derived from the fusion of bioactive quinolone pharmacophore with structurally diverse aryl substituted chromene for its cytotoxicity. Methods: A library of pyrano[3,2-c]quinoline analogues was prepared from one-pot multi component synthesis using various aromatic aldehydes, malononitrile and 2,4-dihydroxy-1-methylquinoline. The new synthetics were primarily screened for its cytotoxicity (IC50) against different human cancer cell lines in vitro. The promising synthetics were further evaluated in vitro for their potency against different kinase activity. The promising compounds were finally tested for their in vivo efficacy in SCID type mice HCT-116 tumor model. Results: The screening results revealed that compounds 4c, 4f, 4i and 4j showed promising activity in in vitro study. However, compound 4c was found to be the most potent candidate with 23% tumor growth inhibition in HCT-116 tumor mice model. Conclusion: The structure activity relationship suggested that 3-substitution on the aryl ring at C4 position of the pyrano[3,2 c]quinolone moiety seems to have an important position for cytotoxicity activity. However, 3- chloro substitution at C4 aryl ring showed a significant alteration of the bioactive conformer of the parent scaffold and outcome with compound 4c as the most potent candidate of the series.

scholarly journals In Vitro Cytotoxic Activity of Origanum vulgare L. on HCT-116 and MDA-MB-231 Cell Lines

Plants ◽  
2013 ◽  
Vol 2 (3) ◽  
pp. 371-378 ◽  
Author(s):  
Filip Grbović ◽  
Milan Stanković ◽  
Milena Ćurčić ◽  
Nataša Đorđević ◽  
Dragana Šeklić ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Origanum Vulgare ◽  
Hct 116

scholarly journals Mutagenicity evaluation of Anastatica hierochuntica L. aqueous extract in vitro and in vivo

2017 ◽  
Vol 243 (4) ◽  
pp. 375-385 ◽  
Author(s):  
Siti Rosmani Md Zin ◽  
Zahurin Mohamed ◽  
Mohammed A Alshawsh ◽  
Won F Wong ◽  
Normadiah M Kassim
Keyword(s):  
Aqueous Extract ◽  
Positive Control ◽  
In Vitro Assay ◽  
In Vivo Study ◽  
Sufficient Evidence ◽  
Aqueous Extracts ◽  
Mutagenic Potential ◽  
Vitro Assay

Anastatica hierochuntica L. ( A. hierochuntica), a folk medicinal plant, was evaluated for mutagenic potential via in vitro and in vivo assays. The in vitro assay was conducted according to modified Ames test, while the in vivo study was performed according to Organisation for Economic Co-operation and Development guideline for mammalian erythrocyte micronucleus assay. Four groups ( n= 5 males and 5 females per group) Sprague Dawley rats were randomly chosen as the negative control, positive control (received a single intramuscular injection of cyclophosphamide 50 mg/kg), 1000 and, 2000 mg/kg A. hierochuntica aqueous extracts. All groups except the positive control were treated orally for three days. Findings of the in vitro assay showed mutagenic potential of AHAE at 0.04 and 0.2 mg/ml. However, no mutagenic effect was demonstrated in the in vivo study up to 2000 mg/kg. No significant reduction in the polychromatic and normochromatic erythrocytes ratio was noted in any of the groups. Meanwhile, high micronucleated polychromatic erythrocytes frequency was seen in cyclophosphamide-treated group only. These findings could perhaps be due to insufficient dosage of A. hierochuntica aqueous extracts to cause genetic damage on the bone marrow target cells. Further acute and chronic in vivo toxicity studies may be required to draw pertinent conclusion on the safety aspect of A. hierochuntica aqueous extracts consumption. Impact statement In this paper, we report on the mutagenicity evaluation of Anastatica hierochuntica aqueous extract. This is a significant research in view of the popularity of this herb consumption by the people across the globe despite of limited scientific evidence on its toxicity potential. This study is intended to encourage more extensive related research in order to provide sufficient evidence and guidance for determining its safe dosage.

scholarly journals Phytochemical Characterization and Evaluation of Biological Activities of Egyptian Carob Pods (Ceratonia siliqua L.) Aqueous Extract: In Vitro Study

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2626
Author(s):  
Wael Sobhy Darwish ◽  
Abada El Sayed Khadr ◽  
Maher Abd El Naby Kamel ◽  
Mabrouk A. Abd Eldaim ◽  
Ibrahim El Tantawy El Sayed ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Phytochemical Analysis ◽  
Type I ◽  
Hypotonic Solution ◽  
Ceratonia Siliqua

Ceratonia siliqua (Carob) is an evergreen Mediterranean tree, and carob pods are potentially nutritive and have medicinal value. The present study was carried out to estimate the possible biological activities of phytochemical-characterized carob pod aqueous extract (CPAE). The phytochemical contents of CPAE were determined by using colorimetric methods and HPLC. In addition, the free radical scavenging properties and anti-diabetic, anti-hemolytic, and antimicrobial activities were estimated by using standardized in vitro protocols. The phytochemical analysis revealed that CPAE was rich in polyphenols, flavonoids, and alkaloids, where it contained a significant amount of gallic acid, catechin, and protocatechuic acid. Furthermore, CPAE exhibited strong antioxidant activity where it prevented the formation of 2, 2-Diphenyl-1-picryl hydrazyl, hydroxyl, and nitric oxide free radicals. Additionally, it had a potent inhibitory effect against digestive enzymes (amylase, maltase, sucrase, and lactase). Moreover, CPAE exhibited anti-Staph aureus, anti-Escherichia coli, anti-Candida albicans, and anti-herpes simplex type I virus (HSV-I). Finally, CPAE protected the erythrocyte membrane from hypotonic solution-induced hemolysis. Altogether, CPAE could be regarded as an interesting source of biologically active antioxidant, anti-diabetic, and antimicrobial preparation for a potential application in pharmaceutical and food supplement fields.

scholarly journals Study the Effects of Olive Leaves Extracts in the activity of the enzyme GOT and their Biological Activities

2017 ◽  
Vol 14 (1) ◽  
pp. 48-59
Author(s):  
Baghdad Science Journal
Keyword(s):  
Aqueous Extract ◽  
Large Scale ◽  
Chemical Elements ◽  
Biological Activities ◽  
Olive Tree ◽  
Food Preservation ◽  
The Body ◽  
Aqueous Extracts ◽  
Olive Leaf ◽  
Olive Leaves

The olive tree, has been used it is important plant for the time being some of their parts on a large scale in the treatment of gastrointestinal disorders and stimulate circulation . Moreover, it is used as antibacterial material and also to address some of the respiratory system, diabetes, food preservation osteoporosis. This study involved the collection of olive leaves from different areas in Baghdad / Iraq. These leaves have been harvested, wash it, then dried and crushed, where the study aimed to identify the active ingredients and chemical elements in the olive leaf as well as its effect on the action of GOT enzyme .The study showed that the aqueous extracts (cold and hot) of the olive leaves powder are acidic in nature pH values are of (5.74 and 5.40) for the aqueous extracts hot and cold respectively. Study revealed the extract contain the a collection of Glycosides, tannins, phenolic compounds, resins, flavonoids, alkaloids, terpenes and compound Alaolurobin. The study also showed ability to activate the enzyme GOT in cold aqueous extract (8.36%). and the percentage (27.35%) of hot aqueous extract. That can be analyzed to the presence of higher concentrations of the active compounds in hot aqueous extract compared with cold aqueous extract especially tannins working to activate enzymes carrier in the cell membrane in the body. The study showed that the analysis of thin layer chromatography, liquid high-performance, ( TLC, HPLC) in extract compounds of phenols olive leaf using a mixture (chloroform, acetic acid) and a 2:5 was more impact in the Gram-positive Staphylococcus aureus, while less impact in a negative Gram Salmonella typhimurium. As proved accurate analysis of the chemical elements in powder of plant leaf olive tree and at different concentrations contain of chemical elements Major estimated by (g /kg) and trace estimated by (mg/kg). Since the existence of these elements led to increasing of enzymatic effectiveness through an increase process of activity the enzyme (GOT), which plays role of important in our bodies being gives indication of the nature of the work and effectiveness of the activity of some members of the body (liver, kidney, pancreas, etc.).

scholarly journals Metabolic Profile and Evaluation of Biological Activities of Extracts from the Stems of Cissus trifoliata

2020 ◽  
Vol 21 (3) ◽  
pp. 930
Author(s):  
Luis Fernando Méndez-López ◽  
Elvira Garza-González ◽  
María Yolanda Ríos ◽  
M. Ángeles Ramírez-Cisneros ◽  
Laura Alvarez ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Antibacterial Activity ◽  
Cytotoxic Activity ◽  
Metabolic Profile ◽  
Biological Activities ◽  
Cytotoxic Activities ◽  
Aqueous Extracts ◽  
Antitumor Effects ◽  
Anticancer Compounds ◽  
High Cytotoxic Activity

Cissus trifoliata (L.) L belongs to the Vitaceae family and is an important medicinal plant used in Mexico for the management of infectious diseases and tumors. The present study aimed to evaluate the metabolic profile of the stems of C. trifoliata and to correlate the results with their antibacterial and cytotoxic activities. The hexane extract was analyzed using gas chromatography coupled with mass spectrometry (GC-MS) and the CHCl3-MeOH and aqueous extracts by ultraperformance liquid chromatography quadrupole time of fly mass spectrometry (UPLC-QTOF-MS). The antibacterial activity was determined by broth microdilution and the cytotoxicity was evaluated using MTS cell proliferation assay. Forty-six metabolites were putatively identified from the three extracts. Overall, terpenes, flavonoids and stilbenes characterize the metabolic profile. No antibacterial activity was found in any extract against the fifteen bacteria strains tested (MIC >500 µg/mL). However, high cytotoxic activity (IC50 ≤ 30 µg/mL) was found in the hexane and aqueous extracts against hepatocarcinoma and breast cancer cells (Hep3B, HepG2 and MCF7). This is the first report of the bioactive compounds of C. trifoliata stems and their antibacterial and cytotoxic properties. The metabolic profile rich in anticancer compounds correlate with the cytotoxic activity of the extracts from the stems of C. trifoliata. This study shows the antitumor effects of this plant used in the traditional medicine and justifies further research of its anticancer activity.

scholarly journals In vitro cytotoxic activity of aqueous extract of Delonix elata (L.) gamble (fabaceae) leaves on mcf-7 & hep g-2 cell lines

2014 ◽  
Vol 2 (2) ◽  
Author(s):  
Phani Kumar Kola ◽  
Shyam Prasad K ◽  
Lakshmi Sudeepthi N ◽  
R.CH.Sekhara Reddy D ◽  
Abdul Rahaman Sk ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Aqueous Extract ◽  
Mcf 7

scholarly journals Physico-chemical and biological studies of Cu(II), Co(II) and Ni(II) complexes of an N4 coordinating ligand derived from diacetylbisethylenediamine and benzoic acid

2012 ◽  
Vol 77 (5) ◽  
pp. 627-637 ◽  
Author(s):  
Pal Singh ◽  
Nanda Srivastava
Keyword(s):  
Benzoic Acid ◽  
Metal Complexes ◽  
Magnetic Moment ◽  
Biological Activities ◽  
Molar Conductance ◽  
Planar Geometry ◽  
Cyclic Voltammetric Study ◽  
Biological Studies ◽  
Antibacterial And Antifungal

Mononuclear metal complexes of the type [ML1]Cl2 (where, M = = Cu(II), Co(II) or Ni(II) and L1 = ligand) were synthesized by the reaction of a new N4 coordinating ligand, derived from diacetylbisethylenediamine with benzoic acid, and the corresponding hydrated metal chloride salts. The metal complexes were characterized by elemental analysis, melting point determination, molar conductance and magnetic moment measurements, IR, UV-Vis, 1H- and 13C-NMR, and ESR spectroscopy. The ligand and all the metal complexes were stable in the solid state at room temperature. From the analytical and spectroscopic investigations, the stoichiometry of the complexes was found to be 1:1 (metal:ligand). Based on the electronic spectra and magnetic moment data, the metal complexes had a square planar geometry. The molar conductance values show the 1:2 electrolytic nature of the metal complexes. A cyclic voltammetric study of the Cu(II) metal complex has also performed, which showed one electron quasi-reversible reduction around -0.92 to -1.10 V. In vitro biological activities of the ligand and metal complexes was checked against two bacteria Bacillus subtilis and Escherichia coli and two fungi Aspirgillus niger and A. flavus which showed the antibacterial and antifungal properties of the ligand and its metal complexes.

scholarly journals Phytochemicals and cancer

2007 ◽  
Vol 66 (2) ◽  
pp. 207-215 ◽  
Author(s):  
Ian T. Johnson
Keyword(s):  
Fruits And Vegetables ◽  
Biological Activities ◽  
Human Subjects ◽  
Biological Effects ◽  
Plant Secondary Metabolites ◽  
Biologically Active ◽  
Carcinogenic Activity ◽  
Plant Foods ◽  
Carcinogenic Effects

Epidemiological studies showing a protective effect of diets rich in fruits and vegetables against cancer have focused attention on the possibility that biologically-active plant secondary metabolites exert anti-carcinogenic activity. This huge group of compounds, now collectively termed ‘phytochemicals’, provides much of the flavour and colour of edible plants and the beverages derived from them. Many of these compounds also exert anti-carcinogenic effects in animal models of cancer, and much progress has been made in defining their many biological activities at the molecular level. Such mechanisms include the detoxification and enhanced excretion of carcinogens, the suppression of inflammatory processes such as cyclooxygenase-2 expression, inhibition of mitosis and the induction of apoptosis at various stages in the progression and promotion of cancer. However, much of the research on phytochemicals has been conducted in vitro, with little regard to the bioavailability and metabolism of the compounds studied. Many phytochemicals present in plant foods are poorly absorbed by human subjects, and this fraction usually undergoes metabolism and rapid excretion. Some compounds that do exert anti-carcinogenic effects at realistic doses may contribute to the putative benefits of plant foods such as berries, brassica vegetables and tea, but further research with human subjects is required to fully confirm and quantify such benefits. Chemoprevention using pharmacological doses of isolated compounds, or the development of ‘customised’ vegetables, may prove valuable but such strategies require a full risk–benefit analysis based on a thorough understanding of the long-term biological effects of what are often surprisingly active compounds.

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